HUP0303458A2 - 6-substituted pyrido-pyrimidines, process for their preparation and pharmaceutical compositions containing them - Google Patents
6-substituted pyrido-pyrimidines, process for their preparation and pharmaceutical compositions containing themInfo
- Publication number
- HUP0303458A2 HUP0303458A2 HU0303458A HUP0303458A HUP0303458A2 HU P0303458 A2 HUP0303458 A2 HU P0303458A2 HU 0303458 A HU0303458 A HU 0303458A HU P0303458 A HUP0303458 A HU P0303458A HU P0303458 A2 HUP0303458 A2 HU P0303458A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- cycloalkyl
- group
- heteroalkyl
- aryl
- Prior art date
Links
- -1 6-substituted pyrido-pyrimidines Chemical class 0.000 title abstract 5
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 12
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 10
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 7
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 5
- 125000001188 haloalkyl group Chemical group 0.000 abstract 4
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 2
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 125000001691 aryl alkyl amino group Chemical group 0.000 abstract 1
- 125000001769 aryl amino group Chemical group 0.000 abstract 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000005343 heterocyclic alkyl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Az (I) vagy (II) általános képletű vegyületek vagy gyógyászatilagalkalmas savaddíciós sóik p38 által közvetített rendellenességekkezelésére alkalmazhatók. A képletekben Z jelentése N vagy CH; Wjelentése NR2; X1 jelentése O, NR4 (ahol R4 jelentése hidrogénatomvagy alkilcsoport), S vagy CR5R6 (ahol R5 és R6 jelentése egymástólfüggetlenül hidrogénatom vagy alkilcsoport) vagy C=O; X2 jelentése Ovagy NR7; Ar1 jelentése aril- vagy heteroaril-csoport; R2 jelentésehidrogénatom, alkil-, acil-, alkoxikarbonil- ariloxikarbonil-,heteroalkilkarbonil-, heteroalkoxikarbonil- vagy -R21 -R22 (ahol R21jelentése alkiléncsoport vagy -C(=O)- és R22 jelentése alkil- vagyalkoxicsoport); R1 jelentése hidrogénatom, alkil-, halogén-alkil-,aril-, aralkil-, heteroaril-, heteroaralkil-, cikloalkil-, cikloalkil-alkil-, heteroalkil-helyettesített cikloalkil-, hetero-helyettesítettcikloalkil-, heteroalkil-, cianoalkil-, heterociklikus-,heterociklikus alkil-, R12-SO2-heterocikloamino- (ahol R12 jelentésehalogén-alkil-, aril-, aralkil-, heteroaril- vagy heteroaralkil-csoport), -Y1-C(O)-Y2-R11 (ahol Y1 és Y2 egymástól függetlenül vagynincs jelen vagy alkiléncsoportot jelent és R11 jelentésehidrogénatom, alkil-, halogén-alkil-, hidroxi-, alkoxi-, amino-,monoalkilamino- vagy dialkilamino-csoport), heterociklikus-cikloalkil-alkil- vagy heterociklikus-heteroaril-alkil-csoport; R3 jelentésehidrogénatom, alkil-; cikloalkil-, cikloalkil-alkil-, aril-, aralkil-,halogén-alkil-, heteroalkil-, ciano-alkil-, alkilén-C(O)-R31 (ahol R31jelentése hidrogénatom, alkil-, hidroxi-, alkoxi-, amino-,monoalkilamino- vagy dialkilamino-csoport), amino-, monoalkilamino-,dialkilamino- vagy NR32-Y3-R33 (ahol Y3 jelentése -C(O), -C(O)O-, -C(O)NR34, S(O)2 vagy S(O)2NR35; R32, R34 és R35 jelentése egymástólfüggetlenül hidrogénatom vagy alkilcsoport; és R33 jelentésehidrogénatom, alkil-, cikloalkil-, cikloalkil-alkil-, heteroalkil-vagy adott esetben helyettesített fenilcsoport) vagy acilcsoport; R7jelentése hidrogénatom vagy alkilcsoport; és R8 és R9 jelentéseegymástól függetlenül hidrogénatom, alkil-, aril-, aralkil-,cikloalkil-, cikloalkil-alkil-, heteroalkil-, alkilszulfonil-;arilszulfonil-, -C(O)-R81 (ahol R81 jelentése alkil-, aril-, aralkil-,cikloalkil-, ckloalkil-alkil-, heteroalkil-, alkoxi-, ariloxi-,amino-, mono- vagy dialkilamino-, arilamino- vagy aril-alkil-amino-csoport) vagy R8 és R9 együtt =CR82R83 csoportot képez (ahol R82 ésR83 jelentése egymástól függetlenül hidrogénatom, alkil-, cikloalkil-,cikloalkil-alkil- vagy adott esetben helyettesített fenilcsoport. Atalálmány kiterjed a vegyületek előállítására és ezeket tartalmazógyógyszerkészítményekre is. ÓThe compounds of formula (I) or (II) or their pharmaceutically acceptable acid addition salts can be used for the treatment of disorders mediated by p38. In the formulas, Z is N or CH; W means NR2; X1 is O, NR4 (where R4 is hydrogen or alkyl), S or CR5R6 (where R5 and R6 are independently hydrogen or alkyl) or C=O; X 2 is O or NR 7 ; Ar 1 is aryl or heteroaryl; R2 represents a hydrogen atom, alkyl-, acyl-, alkoxycarbonyl-aryloxycarbonyl-, heteroalkylcarbonyl-, heteroalkoxycarbonyl- or -R21 -R22 (where R21 represents an alkylene group or -C(=O)- and R22 represents an alkyl- or alkoxy group); R1 is hydrogen, alkyl, haloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heteroalkyl-substituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkyl, cyanoalkyl, heterocyclic -, heterocyclic alkyl-, R12-SO2-heterocycloamino- (where R12 is a haloalkyl-, aryl-, aralkyl-, heteroaryl- or heteroaralkyl group), -Y1-C(O)-Y2-R11 (where Y1 and Y2 independently or not present or an alkylene group and R11 is a hydrogen atom, an alkyl, haloalkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino group), heterocyclic-cycloalkyl-alkyl- or heterocyclic-heteroaryl-alkyl group ; R3 is hydrogen atom, alkyl-; cycloalkyl-, cycloalkyl-alkyl-, aryl-, aralkyl-, haloalkyl-, heteroalkyl-, cyanoalkyl-, alkylene-C(O)-R31 (where R31 is a hydrogen atom, alkyl-, hydroxy-, alkoxy-, amino -, monoalkylamino or dialkylamino group), amino-, monoalkylamino-, dialkylamino- or NR32-Y3-R33 (where Y3 is -C(O), -C(O)O-, -C(O)NR34, S (O)2 or S(O)2NR35; R32, R34 and R35 are independently hydrogen or alkyl; and R33 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, heteroalkyl or optionally substituted phenyl) or acyl; R7 is a hydrogen atom or an alkyl group; and R8 and R9 are independently hydrogen, alkyl-, aryl-, aralkyl-, cycloalkyl-, cycloalkylalkyl-, heteroalkyl-, alkylsulfonyl-; arylsulfonyl-, -C(O)-R81 (wherein R81 is alkyl-, aryl- , aralkyl-, cycloalkyl-, cycloalkylalkyl-, heteroalkyl-, alkoxy-, aryloxy-, amino-, mono- or dialkylamino-, arylamino- or arylalkylamino group) or R8 and R9 together form =CR82R83 (where R82 and R83 independently represent a hydrogen atom, an alkyl, cycloalkyl, cycloalkylalkyl or optionally substituted phenyl group. The invention also covers the production of compounds and pharmaceutical preparations containing them.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26837501P | 2001-02-12 | 2001-02-12 | |
| US33465401P | 2001-11-30 | 2001-11-30 | |
| PCT/EP2002/001106 WO2002064594A2 (en) | 2001-02-12 | 2002-02-04 | 6-substituted pyrido-pyrimidines |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| HUP0303458A2 true HUP0303458A2 (en) | 2004-01-28 |
| HUP0303458A3 HUP0303458A3 (en) | 2012-12-28 |
| HU229604B1 HU229604B1 (en) | 2014-02-28 |
Family
ID=26953040
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0303458A HU229604B1 (en) | 2001-02-12 | 2002-02-04 | 6-substituted pyrido-pyrimidines, process for their preparation and pharmaceutical compositions containing them |
Country Status (32)
| Country | Link |
|---|---|
| US (3) | US6696566B2 (en) |
| EP (1) | EP1361880B1 (en) |
| JP (1) | JP4064818B2 (en) |
| KR (1) | KR100639772B1 (en) |
| CN (1) | CN100376571C (en) |
| AR (1) | AR035854A1 (en) |
| AT (1) | ATE305303T1 (en) |
| AU (1) | AU2002256615B2 (en) |
| BR (1) | BRPI0207172B8 (en) |
| CA (1) | CA2434834C (en) |
| CZ (1) | CZ20032416A3 (en) |
| DE (1) | DE60206363T2 (en) |
| DK (1) | DK1361880T3 (en) |
| ES (1) | ES2249574T3 (en) |
| HK (1) | HK1066170A1 (en) |
| HR (1) | HRP20030624B1 (en) |
| HU (1) | HU229604B1 (en) |
| IL (2) | IL156872A0 (en) |
| JO (1) | JO2410B1 (en) |
| MA (1) | MA26993A1 (en) |
| MX (1) | MXPA03007166A (en) |
| MY (1) | MY131518A (en) |
| NO (1) | NO326133B1 (en) |
| NZ (1) | NZ526961A (en) |
| PA (1) | PA8539201A1 (en) |
| PE (1) | PE20020976A1 (en) |
| PL (1) | PL366918A1 (en) |
| RU (1) | RU2269527C2 (en) |
| SK (1) | SK11322003A3 (en) |
| WO (1) | WO2002064594A2 (en) |
| YU (1) | YU63703A (en) |
| ZA (1) | ZA200305938B (en) |
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| DK1361880T3 (en) | 2001-02-12 | 2006-01-23 | Hoffmann La Roche | 6-substituted pyrido-pyrimidines |
| KR20060111716A (en) | 2002-01-22 | 2006-10-27 | 워너-램버트 캄파니 엘엘씨 | 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones |
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| ATE374201T1 (en) * | 2002-08-06 | 2007-10-15 | Hoffmann La Roche | 6-ALKOXYPYRIDOPYRIMIDINES AS INHIBITORS OF P-38 MAP KINASE |
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| NZ541861A (en) * | 2003-02-26 | 2009-05-31 | Sugen Inc | Aminoheteroaryl compounds as protein kinase inhibitors |
| ES2279361T3 (en) * | 2003-04-16 | 2007-08-16 | F. Hoffmann-La Roche Ag | DERIVATIVES OF (6- (FENOXI) -PIRIDO-3,4-DIPIRIMIDIN-2-IL) -AMINE AS INHIBITORS OF P38 KINASA FOR THE TREATMENT OF INFLAMMATORY STATES SUCH AS REUMATOID ARTHRITIS. |
| DK1685131T3 (en) * | 2003-11-13 | 2007-07-09 | Hoffmann La Roche | Hydroxyalkyl-substituted pyrido-7-pyrimidin-7-ones |
| US20090131430A1 (en) * | 2004-11-23 | 2009-05-21 | Palle Venkata P | Pyrido'2,3-dipyrimidines as anti-inflammatory agents |
| US20060142312A1 (en) * | 2004-12-23 | 2006-06-29 | Pfizer Inc | C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones |
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2002
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- 2002-02-04 WO PCT/EP2002/001106 patent/WO2002064594A2/en not_active Application Discontinuation
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- 2002-02-04 AT AT02726103T patent/ATE305303T1/en active
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